(2R,3R,4R)-N-Benzyloxycarbonyl-2-benzyloxymethyl-4-fluoropyrrolidin-3-yl 2,3,6-tri-O-benzyl-4-O-(2,3,4-tri-O-benzyl-6-deoxy-α-D-glucopyranosyl)-α-D-glucopyranoside | 736968-92-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2R,3R,4R)-N-Benzyloxycarbonyl-2-benzyloxymethyl-4-fluoropyrrolidin-3-yl 2,3,6-tri-O-benzyl-4-O-(2,3,4-tri-O-benzyl-6-deoxy-α-D-glucopyranosyl)-α-D-glucopyranoside
• 英文别名: (2R,3R,4R)-N-Benzyloxycarbonyl-2-benzyloxymethyl-4-fluoro-pyrrolidin-3-yl 2,3,6-tri-O-benzyl-4-O-(2,3,4-tri-O-benzyl-6-deoxy-alpha-D-glucopyranosyl)-alpha-D-glucopyranoside；benzyl (2R,3R,4R)-4-fluoro-3-[(2R,3R,4S,5R,6R)-5-[(2R,3R,4S,5R,6R)-6-methyl-3,4,5-tris(phenylmethoxy)oxan-2-yl]oxy-3,4-bis(phenylmethoxy)-6-(phenylmethoxymethyl)oxan-2-yl]oxy-2-(phenylmethoxymethyl)pyrrolidine-1-carboxylate
• CAS: 736968-92-6
• 化学式: C₇₄H₇₈FNO₁₃
• 分子量: 1208.43
• InChiKey: FXFMKWFRXVAXOP-PXHBEACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  11.5
• 重原子数：
  89
• 可旋转键数：
  30
• 环数：
  11.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  131
• 氢给体数：
  0
• 氢受体数：
  14

反应信息

• 作为反应物：
  描述：

  (2R,3R,4R)-N-Benzyloxycarbonyl-2-benzyloxymethyl-4-fluoropyrrolidin-3-yl 2,3,6-tri-O-benzyl-4-O-(2,3,4-tri-O-benzyl-6-deoxy-α-D-glucopyranosyl)-α-D-glucopyranoside 在 palladium hydroxide carbon 氢气 、 ammonium hydroxide 、 desired compound 作用下， 以 甲醇盐酸 为溶剂， 反应 1.17h， 以to obtain the desired title compound (26 mg, 65%) as a colorless solid的产率得到(2R,3R,4R)-4-fluoro-2-hydroxymethyl-pyrrolidin-3-yl 4-0-(6-deoxy-α-D-glucopyranosyl)-α-D-glucopyranoside
  参考文献：
  名称：

  Oligosaccharide Derivative

  摘要：

  具有式(I)的化合物：其中A表示环状基团，R1和R2表示烷基或羟甲基等基团，n表示1或2，或其药学上可接受的盐或酯，在活性和稳定性方面具有优越性，可用于治疗和/或预防糖尿病等疾病。

  公开号：

  US20080194495A1
• 作为产物：
  描述：

  、 (2R,3R,4R)-N-Benzoyloxycarbonyl-2-benzyloxymethyl-4-fluoropyrrolidine 在 trimethylsilyl trifluoromethanesulfonate 、 三乙胺 作用下， 以 乙醚 为溶剂， 反应 1.5h， 以6%的产率得到(2R,3R,4R)-N-Benzyloxycarbonyl-2-benzyloxymethyl-4-fluoropyrrolidin-3-yl 2,3,6-tri-O-benzyl-4-O-(2,3,4-tri-O-benzyl-6-deoxy-α-D-glucopyranosyl)-α-D-glucopyranoside
  参考文献：
  名称：

  EP1792620

  摘要：

  公开号：

文献信息

• Oligosaccharide derivative
  申请人：Honda Takeshi

  公开号：US20060025350A1

  公开（公告）日：2006-02-02

  Compounds having the formula (I): wherein A represents a group such as a cyclic group, R 1 and R 2 represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.

  具有化学式（I）的化合物：其中A代表环状基团，R1和R2代表烷基或羟甲基等基团，n代表1或2，或其药学上可接受的盐或酯具有卓越的活性和稳定性，并且可用于治疗和/或预防糖尿病等疾病。
• Medicinal Composition Containing Diabeted Remedy
  申请人：Izumi Masanori

  公开号：US20080039367A1

  公开（公告）日：2008-02-14

  A pharmaceutical composition effective for the prophylaxis and treatment of diabetes is provided. This pharmaceutical composition comprises the combination of an α-amylase inhibitor selected from a compound represented by the following general formula (I): [wherein A represents, for example, a cyclic group, etc. R 1 and R 2 represent an alkyl group, hydroxymethyl group, etc., and n represents 1 or 2], or a pharmacologically acceptable salt or ester thereof, and at least one type of drug selected from an insulin sensitizer, an insulin secretagogue, a biguanide drug, an insulin preparation and a DPP-IV inhibitor.

  提供一种用于预防和治疗糖尿病的药物组合物。该药物组合物包括以下通用式（I）所表示的化合物中选择的α-淀粉酶抑制剂：[其中A代表环状基团等，R1和R2代表烷基、羟甲基基团等，n代表1或2]，或其药理学上可接受的盐或酯，以及选择自胰岛素增敏剂、胰岛素分泌促进剂、双胍类药物、胰岛素制剂和DPP-IV抑制剂中的至少一种药物。
• MEDICINAL COMPOSITION CONTAINING DIABETES REMEDY
  申请人：Sankyo Company, Limited

  公开号：EP1792620A1

  公开（公告）日：2007-06-06

  A pharmaceutical composition effective for the prophylaxis and treatment of, diabetes is provided. This pharmaceutical composition comprises the combination of an α-amylase inhibitor selected from a compound represented by the following general formula (I): [wherein A represents, for example, a cyclic group, etc. R1 and R2 represent an alkyl group, hydroxymethyl group, etc., and n represents 1 or 2], or a pharmacologically acceptable salt or ester thereof, and at least one type of drug selected from an insulin sensitizer, an insulin secretagogue, a biguanide drug, an insulin preparation and a DPP-IV inhibitor.

  本发明提供了一种有效预防和治疗糖尿病的药物组合物。这种药物组合物包括一种α-淀粉酶抑制剂，该抑制剂选自以下通式（I）所代表的化合物： [其中 A 代表环状基团等。 R1和R2代表烷基、羟甲基等，n代表1或2]，或其药理上可接受的盐或酯，以及至少一种选自胰岛素增敏剂、胰岛素促泌剂、双胍类药物、胰岛素制剂和DPP-IV抑制剂的药物。
• OLIGOSACCHARIDE DERIVATIVE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP1589023B1

  公开（公告）日：2010-08-25
• US7361744B2
  申请人：——

  公开号：US7361744B2

  公开（公告）日：2008-04-22